Scalarane Sesterterpenes from a Marine Sponge of the Genus Spongia and Their FXR Antagonistic Activity
Journal of Natural Products2007Vol. 70(11), pp. 1691–1695
Citations Over TimeTop 11% of 2007 papers
Sang‐Jip Nam, Hyunsil Ko, Moon Kyeong Ju, Hoosang Hwang, Jungwook Chin, Jungyeob Ham, Byoungchan Lee, John J. Lee, Dong Hwan Won, Hyukjae Choi, Jaeyoung Ko, Kyoungjin Shin, Taekyung Oh, Seokho Kim, Jung‐Rae Rho, Heonjoong Kang
Abstract
Three new scalarane-based sesterterpenes, 1- 3, were isolated from a marine sponge of the genus Spongia, and their chemical structures were elucidated by analysis of HRMS and 2-D NMR spectra. The isolated compounds 1 and 3 showed inhibition against the farnesoid X-activated receptor (FXR) with IC50 values of 2.4 and 24 microM, respectively. In particular, compound 3 directly inhibited the interaction between FXR and a coactivator peptide (SRC-1) as determined by surface plasmon resonance (SPR) spectroscopy.
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